[<SUP>99m</SUP>Tc]Tc-HYNIC-EcgDf21: A defensin short analogue with potential application in infection foci imaging

作     者：Teran, Mariella Osorio, Jessica Cardoso, Elena Tejeria, Emilia Paolino, Andrea Reyes, Ana Laura Cecchetto, Gianna 

作者机构：Univ Republ Udelar Fac Quim Dept Estrella Campos Area Radioquim Estrella Campos Montevideo Uruguay Ctr Uruguayo Imagenol Mol CUDIM Montevideo Uruguay Univ Republ Udelar Fac Quim Fac Ciencias Inst Quim BiolDept BiocienciasArea Microbiologl Montevideo Uruguay 

出 版 物：《CHEMICAL BIOLOGY & DRUG DESIGN》 (化学生物学与药物研制)

年 卷 期：2023年第101卷第3期

页      面：593-604页

核心收录：

学科分类：0710[理学-生物学] 1007[医学-药学(可授医学、理学学位)] 071010[理学-生物化学与分子生物学] 07[理学] 

基　　金：Comision Sectorial de Investigacion Cientifica PEDECIBA Comision Sectorial de Investigacion Cientifica Universidad de la Republica (CSIC) 

主　　题：A niger C albicans Ceibo defensins Erythrina crista-galli infection peptides radiolabelling S aureus SPECT tracers technetium 99m 

摘      要：Opportunistic infections are a problem of great relevance in public health and the precise detection and localization of infection in the early stages of the disease is of great importance for patient management as well as cost containment. Our proposal seeks to contribute to developing a new agent that meets the needs of diagnosis and follow-up of fungal and bacterial infections, focused on the design of a radiotracer with the potential for recognition of hidden infection foci. Defensins are plant antimicrobial peptides that not only show activity against plant pathogens but also against human ones. A short analogue of EcgDf1 defensin, EcgDf21d (NH2-ERFTGGHCRGFRRRCFCTKHC-COOH), was labelled through the formation of a Tc-99m-HYNIC complex which was assessed for physicochemical and biological behaviour both in vitro and in vivo. The [Tc-99m]Tc-HYNIC-EcgDf21 labelling procedure rendered a single product with remarkably high RCP and stability in the labelling milieu. The Log p value indicated that [Tc-99m]Tc-HYNIC-EcgDf21 has a hydrophilic behaviour, confirmed by the biodistribution profiles. The optimal uptake value was obtained for Candida albicans infection model reaching a lesion/muscle ratio of 3, this correlates with in vitro binding studies, and the lesion can be definitely observed in the scintigraphic images.